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手性农用化学品的持续重要性。

The continuing significance of chiral agrochemicals.

作者信息

Jeschke Peter

机构信息

Heinrich-Heine-University Düsseldorf, Institute of Organic Chemistry and Macromolecular Chemistry, Duesseldorf, Germany.

出版信息

Pest Manag Sci. 2025 Apr;81(4):1697-1716. doi: 10.1002/ps.8655. Epub 2025 Jan 17.

Abstract

Chemical crop protection is one of the most cost-effective methods for agriculture, as crop failures can be prevented, and sustainable growth can be enabled regardless of the seasons. Agricultural production must be significantly increased in the future to meet the food needs of a growing world population. However, the continued loss of established active ingredients due to consumer perceptions, changing needs of farmers and ever-changing regulatory requirements is higher than annually new active ingredients introduced to the market. The development of innovative active ingredients is therefore essential to continuously improve the selectivity, efficacy and favorable environmental profile of agrochemicals. Molecules with stereogenic centers can be considered here, as they often have different properties than non-chiral molecules. Natural products and their congeners are still a valuable source of inspiration for chiral agrochemicals. However, only a few novel chiral agrochemicals are currently produced on an industrial scale as pure stereoisomers or in enriched form. As of 2018, around 43% of the 35 chiral products introduced to the market (herbicides, fungicides, insecticides, acaricides, and nematicides) contain one or more stereogenic centers in the molecule, and almost 69% of them have been marketed as racemic mixtures of enantiomers or stereoisomers. Surprisingly, the proportion of chiral agrochemicals is in the same order of magnitude as in the time frame from 2007 to 2017 with around 42%, respectively. This report therefore provides an overview of the continued importance of chiral agrochemicals brought to market in the last 6 years and describes the inherent related challenges of modern agrochemicals through the management of key aspects arising from innovative crop protection products. © 2025 The Author(s). Pest Management Science published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.

摘要

化学作物保护是农业中最具成本效益的方法之一,因为它可以预防作物歉收,并且无论季节如何都能实现可持续增长。为满足不断增长的世界人口的粮食需求,未来必须大幅提高农业产量。然而,由于消费者认知、农民需求的变化以及监管要求的不断变化,现有活性成分的持续流失速度高于每年推向市场的新活性成分。因此,开发创新型活性成分对于持续提高农用化学品的选择性、功效和良好的环境特性至关重要。在此可以考虑具有立体中心的分子,因为它们的性质通常与非手性分子不同。天然产物及其类似物仍然是手性农用化学品的宝贵灵感来源。然而,目前只有少数新型手性农用化学品以纯立体异构体或富集形式进行工业规模生产。截至2018年,推向市场的35种手性产品(除草剂、杀菌剂、杀虫剂、杀螨剂和杀线虫剂)中,约43%的分子含有一个或多个立体中心,其中近69%以对映体或立体异构体的外消旋混合物形式销售。令人惊讶的是,手性农用化学品的比例与2007年至2017年期间的数量级相同,分别约为42%。因此,本报告概述了过去6年推向市场的手性农用化学品的持续重要性,并通过管理创新作物保护产品产生的关键方面描述了现代农用化学品固有的相关挑战。© 2025作者。由John Wiley & Sons Ltd代表化学工业协会出版的《害虫管理科学》。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/62fb/11906909/5bfddd78de87/PS-81-1697-g004.jpg

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